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Synthesis and evaluation of novel monosubstituted sulfonylurea derivatives as antituberculosis agents. 2012
Li Pan, and
Ying Jiang, and
Zhen Liu, and
Xing-Hai Liu, and
Zhuo Liu, and
Gang Wang, and
Zheng-Ming Li, and
Di Wang
State-Key Laboratory of Elemento-Organic Chemistry, National Pesticide Engineering Research Center(Tianjin), Nankai University, Tianjin 300071, China.
A series of novel monosubstituted sulfonylurea derivatives 10a-y were synthesized and characterized by (1)H NMR, (13)C NMR and HRMS. These compounds were evaluated against Mycobacterium tuberculosis H37Rv in vitro. The results showed compounds 10f, 10k and 10s exhibited moderate antituberculosis activities with MIC values in the range of 20-100 mg/L. Compounds 10b and 10o displayed good antituberculosis activities (MIC 10 mg/L), which were comparable with that of the sulfometuron methyl. Both of the two compounds showed little cytotoxicities, with an IC(50) against THP-1 cells greater than 100 mg/L.
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